摘要
α-芳基膦酸酯作为一类重要的有机膦化合物,在药物化学中具有重要应用价值;同时,香豆素和喹啉酮也是该领域十分常见的骨架结构.然而,目前α-膦酸化的香豆素/喹啉酮及其衍生物的合成方法十分有限.为此,开发了一种可见光驱动下卤键诱导的直接偶联反应,实现了α-碘甲基膦酸二乙酯与香豆素或喹啉酮的高效连接.该反应条件温和、操作简便,且具有优异的底物普适性和区域选择性.
α-Aryl phosphonates represent an important class of organophosphorus compounds with significant application value in medicinal chemistry.Meanwhile,coumarin and quinolinone are ubiquitous scaffold structures in this field.However,synthetic methods forα-phosphonylated coumarin/quinolinone derivatives remain limited.To address this,a visible-lightdriven,halogen-bond-induced direct coupling reaction was developed,enabling the efficient covalent linkage between diethylα-iodomethylphosphonate and coumarin or quinolinone.This transformation features mild reaction conditions,simple operation,excellent substrate compatibility,and high regioselectivity.
作者
梁家瑞
李金兰
蒋云
姚秋丽
徐应淑
王安俊
Liang Jiarui;Li Jinlan;Jiang Yun;Yao Qiuli;Xu Yingshu;Wang Anjun(Guizhou Provincial Key Laboratory of Innovation and Manufacturing for Pharmaceuticals,School of Pharmacy,Zunyi Medical University,Zunyi,Guizhou 563000)
出处
《有机化学》
北大核心
2026年第1期135-145,共11页
Chinese Journal of Organic Chemistry
基金
合肥市科技计划(No.遵市科合HZ字(2023)169)
贵州省科技计划(No.黔科平台人才[2021]1350-005)
贵州省科学技术厅(No.黔科合平台人才-CXTD[2022]012)资助项目.
